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GW-311616 is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).

GW-311616 is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 2 mg | 待询 | 5日内发货 | |
| 25 mg | 待询 | 10-14周 | |
| 50 mg | 待询 | 10-14周 | |
| 100 mg | 待询 | 10-14周 |
| 产品描述 | GW-311616 is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM). |
| 靶点活性 | HNE:(ki)0.31 nM , HNE:22 nM |
| 体外活性 | GW-311616 (150 μM;?U937 cells) treatment can increase the protein expression levels of Bax and decrease the expression of Bcl-2.GW-311616 (150 μM; 48 hours) markedly suppresses NE activity in U937 and K562 cells lines. GW-311616 (20-320 μM; 48 hours; U937 cells) treatment inhibits proliferation and induces apoptosis in leukemia cells. |
| 体内活性 | GW-311616 has moderate terminal elimination half-life (t1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively.GW-311616 (2 mg/kg;?oral administration) rapidly abolishes the circulation of neutrophil elastase (NE) in dogs, while >90% inhibition is maintained for 4 days.?This prolonged effect is independent to be due to penetration of neutrophils in bone marrow by orally administrated GW-311616. |
| 分子量 | 397.53 |
| 分子式 | C19H31N3O4S |
| CAS No. | 198062-54-3 |
| Smiles | [H][C@@]12CCN(C(=O)\C=C\CN3CCCCC3)[C@@]1([H])[C@H](C(C)C)C(=O)N2S(C)(=O)=O |
| 密度 | 1.27 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 44 mg/mL (110.68 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (5.03 mM), Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多